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A series of 2-arylamino-5-(indolyl)-1,3,4-thiadiazoles as potent cytotoxic agents

Authors
Journal
European Journal of Medicinal Chemistry
0223-5234
Publisher
Elsevier
Volume
55
Identifiers
DOI: 10.1016/j.ejmech.2012.06.047
Keywords
  • 2-Arylamino-1
  • 3
  • 4-Thiadiazoles
  • Indolyl Heterocycles
  • Cytotoxic Agents
  • 1
  • 3
  • 4-Thiadiazoles
Disciplines
  • Biology

Abstract

Abstract A series of 2-arylamino-5-(indolyl)-1,3,4-thiadiazoles 6a–v were prepared and studied for their anticancer activity against selected human cancer cell lines. The reaction of indolylhydrazides 3a–h with a variety of aryl isothiocyanates 4 afforded the key intermediate thiosemicarbazides 5a–v, which upon treatment with acetyl chloride produced the 2-arylamino-5-(indolyl)-1,3,4-thiadiazoles 6a–v in good yields. Most of the synthesized compounds showed selective cytotoxicity towards human breast cancer cell line (MDA-MB-231). Of the synthesized 2-arylamino-5-(indolyl)-1,3,4-thiadiazoles, compound 6f is the most potent towards tested cancer cell lines (IC50 = 0.15–1.18 μM).

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